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Rolled into one 3,75 mg of a buserelin (3,93 mg of a buserelin acetate) – active ingredient contain.
- 2 mg — polysorbate 80;
- 30 mg — a karmelloza of sodium;
- 85 mg — Mannitolum;
- 200 mg — copolymer of DL milk and glycolic acids.
Mannitol solution in 2 ml of water for injections acts as solvent as 0,8%.
Lyophilisate for further preparation of the suspension (the prolonged action) used for intramuscular introduction. Packaging contains one bottle with lyophilisate complete with a solvent ampoule. Also 1 syringe, 2 needles, 2 spirit tampons is applied.
Pharmacodynamics and pharmacokinetics
Antineoplastic medicine Buserelin-Depo is synthetic analog of GNRG. Competitively contacting cellular receptors of a front share of a hypophysis, leads to short-term increase in contents in a blood plasma of sex hormones.
In 12-14 days of carrying out treatment in therapeutic doses, there is a full blocking of gonadotropic function of a hypophysis and replication of LG and FSG is as a result oppressed. Thanks to these processes synthesis in gonads of sex hormones that leads to lowering in a blood plasma of concentration of oestradiol (to such values which are observed in the postclimacteric period at women) and testosterone is suppressed (to values of the postkastratsionny period at men).
At continuous therapy for 2-3 weeks the content of testosterone decreases to concentration characteristic at a condition of an orkhiektomiya, in other words, drug leads to pharmacological castration.
Buserelin possesses high bioavailability.
Cmax in plasma is observed approximately in 120-180 minutes after an intramuscular injection and remains within 4 weeks at the sufficient level of oppression by a hypophysis of synthesis of gonadotrophins.
Indications to use
- breast cancer;
- hormonedependent prostate cancer (prostate);
- endometriosis (during the preoperative and postoperative periods);
- hyperplastic changes of an endometria;
- therapy of infertility, within the EKO program (extracorporal fertilization).
Central nervous system:
- when carrying out long therapy observed demineralization of a bone tissue (can be the cause of development of osteoporosis).
When carrying out therapy at female patients the following by-effects are possible: a headache, perspiration, a depression, change of a libido, pain in the bottom of a stomach, dryness of a vagina, bleeding as menstrual (generally for the first weeks of therapy).
At therapy of a prostate cancer at men, Buserelin's use can cause progressing or an aggravation of a basic disease (for the first 2-3 weeks after introduction of the first dose). This phenomenon is connected with stimulation of synthesis of gonadotrophins and, as a result of testosterone.
Development of a gynecomastia, the strengthened sweating, inflow, lowering of a potentiality (sometimes demanding treatment review), passing increase in content in blood of androgens, an urination delay, feeling of weakness in the lower extremities, hypostases of legs, a century and persons is also possible.
At the beginning of a therapy course at patients with a prostate cancer the strengthening of pain in bones, a temporality which is the indication for carrying out a symptomatic treatment can be shown.
Separate episodes of squeezing of a spinal cord and development of impassability of ureters were noted.
Very seldom observed dispeptic frustration and a thromboembolism of a pulmonary artery.
Application instruction (Way and dosage)
Drug Buserelin is intended to depot only for intramuscular introduction.
At therapy of a hormonedependent prostate cancer drug Buserelin of depot, the instruction recommends carrying out intramuscular injections in a dose of 3,75 mg appointed each 4 weeks.
For treatment of hyperplastic changes of an endometria and endometriosis drug appoint 3,75 mg in a dose. Injections are given intramusculary once, by each 4 weeks. The beginning of therapy should be combined with the first five days of a menstrual cycle. The course of treatment makes from 4th to 6 months.
Therapy of a hysteromyoma is carried out in a dose of 3,75 mg of Buserelin entered once intramusculary each 4 weeks. The application instruction recommends to begin treatment in the first five days of a menstrual cycle. The course of carrying out therapy before an operative measure makes 3 months, is equal in other cases to 6 months.
Treatment of infertility determines a single dose of drug by the EKO program — 3,75 mg. An injection carry out at the beginning of a follikulinovy phase (second day of a menstrual cycle) or closer to the end of a lyuteinovy phase (the 21-24th days of a menstrual cycle), before stimulation. For 12-15 day after an injection determine the content of estrogen which has to be lowered for 50% and more initial level in blood serum. In the absence of other contraindications carry out stimulation of a superovulation by means of gonadotropic hormones. Procedure is carried out under control of concentration of oestradiol in blood and with use of ultrasonic monitoring.
Preparations of suspension it can be carried out only by the experienced health worker with use of solvent and other components (needles, the syringe, the spirit tampons) which are included in the drug packaging package.
Ready suspension should be used immediately after its preparation.
Today overdose cases Buserelin the depot was not observed by medicine.
The combined Buserelin-Depo's use with medicines which contain sex hormones can provoke development of a syndrome of hyper stimulation of ovaries.
Pi simultaneous use of hypoglycemic means and Buserelin, efficiency of the first can decrease.
Terms of sale
According to the recipe.
Drug Buserelin-Depo belongs to the list B.
It is necessary to store in the dark, unavailable place for children, at a temperature from 8 ° up to 20 °C.
Period of validity
In case of diagnosing at the patient of any form of a depression or suspicion on it, during therapy with Buserelin's use it has to be under continuous supervision of the attending physician.
The induction of an ovulation is carried out under strict supervision from medical personnel.
At the beginning of therapy forming of an oothecoma is possible.
Before purpose of therapy by drug of Buserelin-depot it is necessary to exclude possible pregnancy then to stop reception of hormonal contraceptive means (if those were used). However, for the first two months of treatment it is necessary to use other efficient methods of contraception, for the purpose of prevention of undesirable pregnancy during this period.
In the first phase of action of Buserelin, for the purpose of prevention of probable side effects, purpose of the anti-androgens applied in 14 days prior to the first injection and also for 14 days after it is necessary.
Coincidence on the ATH code of the 4th level:
Analogs of medicine of Buserelin-depot are provided by the following drugs:
It is worth remembering that independently to select analogs, substitutes of medicines it is not recommended, in particular that which are used for carrying out antineoplastic therapy and at treatment of other serious diseases.
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